ZA200803820B - Pharmaceutical salts and polymorphs of N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino) iminomethyl] benzoyl] amino]-5-meth oxy-benzamide, A factor Xa inhibitor - Google Patents

Pharmaceutical salts and polymorphs of N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino) iminomethyl] benzoyl] amino]-5-meth oxy-benzamide, A factor Xa inhibitor

Info

Publication number
ZA200803820B
ZA200803820B ZA200803820A ZA200803820A ZA200803820B ZA 200803820 B ZA200803820 B ZA 200803820B ZA 200803820 A ZA200803820 A ZA 200803820A ZA 200803820 A ZA200803820 A ZA 200803820A ZA 200803820 B ZA200803820 B ZA 200803820B
Authority
ZA
South Africa
Prior art keywords
iminomethyl
polymorphs
benzamide
pyridinyl
dimethylamino
Prior art date
Application number
ZA200803820A
Inventor
Grant Craig
Langlands Graeme
James P Kanter
Original Assignee
Millennium Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of ZA200803820B publication Critical patent/ZA200803820B/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/194Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/60Salicylic acid; Derivatives thereof
    • A61K31/612Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
ZA200803820A 2005-11-08 2008-05-05 Pharmaceutical salts and polymorphs of N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino) iminomethyl] benzoyl] amino]-5-meth oxy-benzamide, A factor Xa inhibitor ZA200803820B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US73522405P 2005-11-08 2005-11-08

Publications (1)

Publication Number Publication Date
ZA200803820B true ZA200803820B (en) 2009-03-25

Family

ID=38023988

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200803820A ZA200803820B (en) 2005-11-08 2008-05-05 Pharmaceutical salts and polymorphs of N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino) iminomethyl] benzoyl] amino]-5-meth oxy-benzamide, A factor Xa inhibitor

Country Status (21)

Country Link
US (7) US7598276B2 (en)
EP (2) EP1948608B1 (en)
JP (2) JP5227178B2 (en)
KR (1) KR101358574B1 (en)
CN (2) CN102336702B (en)
AR (2) AR056787A1 (en)
AT (1) ATE549317T1 (en)
AU (1) AU2006311544B2 (en)
BR (1) BRPI0618362A2 (en)
CA (1) CA2627086C (en)
DK (1) DK1948608T3 (en)
ES (1) ES2384116T3 (en)
HK (1) HK1115131A1 (en)
IL (2) IL190524A (en)
NZ (2) NZ567992A (en)
PE (2) PE20070717A1 (en)
PT (1) PT1948608E (en)
RU (1) RU2440986C2 (en)
TW (1) TWI443088B (en)
WO (1) WO2007056517A2 (en)
ZA (1) ZA200803820B (en)

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US8394964B2 (en) 2009-12-17 2013-03-12 Millennium Pharmaceuticals, Inc. Methods of synthesizing factor Xa inhibitors
WO2011075602A1 (en) * 2009-12-17 2011-06-23 Millennium Pharmaceuticals, Inc. Methods of preparing factor xa inhibitors and salts thereof
CA2784921A1 (en) * 2009-12-17 2011-07-14 Millennium Pharmaceuticals, Inc. Salts and crystalline forms of a factor xa inhibitor
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AR082804A1 (en) * 2010-09-01 2013-01-09 Portola Pharm Inc CRYSTAL FORMS OF AN XA FACTOR INHIBITOR
TW201240664A (en) 2010-09-01 2012-10-16 Portola Pharm Inc Methods and formulations of treating thrombosis with betrixaban and a P-glycoprotein inhibitor
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WO2013033370A1 (en) 2011-08-31 2013-03-07 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
US9200268B2 (en) * 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
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CN104341343B (en) * 2013-07-24 2018-09-28 四川海思科制药有限公司 Crystal form of betrixaban and its preparation method and application
CN105085387A (en) * 2014-05-20 2015-11-25 四川海思科制药有限公司 Betrixaban salt, preparation method and application thereof
CN107073082B (en) 2014-08-20 2021-04-30 博尔托拉制药公司 Lyophilized formulations of factor XA antidotes
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EP3419650B1 (en) 2016-02-24 2021-06-02 Alexion Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
WO2017208169A1 (en) * 2016-06-02 2017-12-07 Dr. Reddy’S Laboratories Limited Polymorphs of betrixaban & its maleate salt
EP3254674A1 (en) 2016-06-08 2017-12-13 Sandoz Ag Pharmaceutical compositions of betrixaban maleate
SI3472314T1 (en) 2016-06-17 2021-11-30 Alexion Pharmaceuticals, Inc. Preparation of factor xa derivatives
WO2018042320A1 (en) * 2016-08-30 2018-03-08 Dr. Reddy’S Laboratories Limited Salts of betrixaban and processes for preparation thereof
EP3293174A1 (en) 2016-09-09 2018-03-14 Sandoz Ag Crystalline salts of betrixaban
WO2018069936A1 (en) 2016-10-13 2018-04-19 Mylan Laboratories Limited Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof
CN108017576B (en) * 2016-11-01 2022-06-21 石药集团中奇制药技术(石家庄)有限公司 Preparation method of betrixaban and hydrochloride thereof, and crystal forms of betrixaban and hydrochloride thereof
CN108586325A (en) * 2017-03-16 2018-09-28 上海度德医药科技有限公司 A kind of preparation method of Betrixaban intermediates
WO2018229796A2 (en) * 2017-06-14 2018-12-20 Mylan Laboratories Limited A process for betrixaban hydrochloride and betrixaban maleate salt
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Also Published As

Publication number Publication date
TW200736221A (en) 2007-10-01
IL213487A0 (en) 2011-07-31
ATE549317T1 (en) 2012-03-15
HK1115131A1 (en) 2008-11-21
KR20080065662A (en) 2008-07-14
US8557852B2 (en) 2013-10-15
US20130064806A1 (en) 2013-03-14
CN101304971B (en) 2011-09-07
EP1948608A2 (en) 2008-07-30
CN101304971A (en) 2008-11-12
WO2007056517A3 (en) 2008-04-17
AU2006311544B2 (en) 2012-03-08
JP5662980B2 (en) 2015-02-04
US20070112039A1 (en) 2007-05-17
US20170326119A1 (en) 2017-11-16
ES2384116T3 (en) 2012-06-29
IL190524A0 (en) 2008-12-29
KR101358574B1 (en) 2014-02-04
EP1948608B1 (en) 2012-03-14
US20100063113A1 (en) 2010-03-11
IL190524A (en) 2013-02-28
DK1948608T3 (en) 2012-07-02
US9555023B2 (en) 2017-01-31
NZ567992A (en) 2011-05-27
CA2627086A1 (en) 2007-05-18
CN102336702B (en) 2015-02-11
JP5227178B2 (en) 2013-07-03
JP2012246323A (en) 2012-12-13
JP2009514976A (en) 2009-04-09
PE20110070A1 (en) 2011-03-04
WO2007056517A2 (en) 2007-05-18
US9061019B2 (en) 2015-06-23
US20160101089A1 (en) 2016-04-14
RU2008123055A (en) 2009-12-20
CN102336702A (en) 2012-02-01
AU2006311544A1 (en) 2007-05-18
CA2627086C (en) 2016-04-05
US20140288028A1 (en) 2014-09-25
AR056787A1 (en) 2007-10-24
RU2440986C2 (en) 2012-01-27
PE20070717A1 (en) 2007-08-17
BRPI0618362A2 (en) 2011-08-30
EP2431358A1 (en) 2012-03-21
US20190046510A1 (en) 2019-02-14
AR106960A2 (en) 2018-03-07
TWI443088B (en) 2014-07-01
PT1948608E (en) 2012-05-24
US7598276B2 (en) 2009-10-06
NZ592533A (en) 2012-08-31

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